3-ヒドロキシ-2-オキソ-24-ノル-D:A-フリードオレアナ-1(10),3,5,7-テトラエン-29-酸メチル 化学特性,用途語,生産方法
説明
Monoacylglycerol lipase (MAGL) hydrolyzes the endogenous cannabinoid 2-
arachidonoyl glycerol (2-
AG), terminating its capacity to activate cannabinoid receptors. Pristimerin is a naturally occurring terpenoid that potently inhibits MAGL (IC
50 = 93 nM). Its actions are rapid, reversible, and noncompetitive. Pristimerin (1 μM) significantly increases 2-
AG levels in isolated rat neurons, indicating that it inhibits endogenous MAGL in cultured cells. Moreover, it does not increase levels of palmitoyl ethanolamide, suggesting that pristimerin does not affect the activity of fatty acid amide hydrolase (FAAH).
使用
Pristimerin is a triterpenoid that inhibits tumor angiogenesis by targeting VEGFR2 activation and is known to exhibit anti-inflammatory properties.
一般的な説明
A cell-permeable plant dienone-phenolic triterpenoid, naturally isolated from
tripterygium wilfordii, whose inhibitory activities against proteasome chymotrypsin subunit (IC
50 = 2.2 and 3.0 μM against purified rabbit 20S and human 26S proteasome, respectively) and cellular NF-κB pathway/IKK activation most likely account for its reported anticancer efficacy both
in vitro (IC
50 ≤610 nM in A549, K562, KBM5, MCF-7, MDA-MB-231, HepG2, and primary human leukemia cell cultures) and in mice
in vivo (1 to 2.5 mg/kg/day, s.c.), including imatinib/STI571-resistant cancer cells harboring Bcr-Abl T315I mutation. Also reported to inhibit the activity of monoacylglycerol lipase (MGL), the enzyme that hydrolyzes and deactivates the cannabionoid receptor ligand 2-Arachidonoyl-
sn-glycerol (2-AG), in a reversible manner with high potency (IC
50 = 93 nM).
生物活性
Potent and reversible inhibitor of monoacylglycerol lipase (MGL) (IC 50 = 93 nM). Also suppresses NF- κ B activation via inhibition of proteasome chymotrypsin-like activity and IKK α / β . Displays antitumor, anti-inflammatory and antimicrobial activities.
3-ヒドロキシ-2-オキソ-24-ノル-D:A-フリードオレアナ-1(10),3,5,7-テトラエン-29-酸メチル 上流と下流の製品情報
原材料
準備製品